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    Antihypertensive 5-amino-4-hydroxyvaleryl derivatives substituted by sulphur-containing groups
    1.
    发明授权
    Antihypertensive 5-amino-4-hydroxyvaleryl derivatives substituted by sulphur-containing groups 失效
    由含硫基取代的抗高血压5-氨基-4-羟基戊酰基衍生物

    公开(公告)号：US4758584A

    公开(公告)日：1988-07-19

    申请号：US011183

    申请日：1987-02-05

    申请人： Peter Buhlmayer ,  James L. Stanton ,  Walter Fuhrer ,  Richard Goschke ,  Vittorio Rasetti ,  Heinrich Rueger

    发明人： Peter Buhlmayer ,  James L. Stanton ,  Walter Fuhrer ,  Richard Goschke ,  Vittorio Rasetti ,  Heinrich Rueger

    IPC分类号： C07D233/54 ,  C07D401/12 ,  C07D417/12 ,  C07K5/02 ,  A61K37/64 ,  C07K5/08

    CPC分类号： C07D233/64 ,  C07D401/12 ,  C07D417/12 ,  C07K5/0227 ,  Y10S530/86

    摘要： Compounds of the formula ##STR1## in which R.sub.1 represents acyl substituted by a thio, sulphinyl or sulphonyl group, A represents an optionally N-alkylated .alpha.-amino acid residue that is bonded N-terminally to R.sub.1 and C-terminally to the group --NR.sub.2 --, R.sub.2 represents hydrogen or lower alkyl, R.sub.3 represents hydrogen, lower alkyl, optionally etherified or esterified hydroxy-lower alkyl, cycloalkyl, cycloalkyl-lower alkyl, bicycloalkyl-lower alkyl, tricycloalkyl-lower alkyl, aryl or aryl-lower alkyl, R.sub.4 represents hydroxy or etherified or esterified hydroxy, R.sub.5 represents lower alkyl, optionally etherified or esterified hydroxy-lower alkyl, cycloalkyl, cycloalkyl-lower alkyl, bicycloalkyl, bicycloalkyl-lower alkyl, tricycloalkyl, tricycloalkyl-lower alkyl, aryl, aryl-lower alkyl, optionally substituted carbamoyl, optionally substituted amino, optionally substituted hydroxy, optionally substituted mercapto, sulphinyl or sulphonyl, and R.sub.6 represents substituted amino, and salts of such compounds having salt-forming groups, inhibit the blood pressure-increasing action of the enzyme renin and can be used as anti-hypertensives.

    摘要翻译： 式（I）的化合物，其中R 1表示被硫代，亚磺酰基或磺酰基取代的酰基，A表示任选N-烷基化的α-氨基酸残基，其N-末端与R1和C-末端键合 基团-NR 2 - ，R 2表示氢或低级烷基，R 3表示氢，低级烷基，任选醚化或酯化的羟基 - 低级烷基，环烷基，环烷基 - 低级烷基，双环烷基 - 低级烷基，三环烷基 - 低级烷基，芳基或芳基 - 低级烷基，R4代表羟基或醚化或酯化的羟基，R5代表低级烷基，任选醚化或酯化羟基 - 低级烷基，环烷基，环烷基 - 低级烷基，双环烷基，双环烷基 - 低级烷基，三环烷基，三环烷基 - 低级烷基，芳基，芳基 - 低级烷基，任选取代的氨基甲酰基，任选取代的氨基，任选取代的羟基，任选取代的巯基，亚磺酰基或磺酰基，R 6代表取代的氨基， 具有盐形成基团，抑制了肾素素的增压作用，可用作抗高血压药。

    Antihypertensive 5-amino-4-hydroxyvaleryl derivatives substituted by sulphur-containing groups
    4.
    发明授权
    Antihypertensive 5-amino-4-hydroxyvaleryl derivatives substituted by sulphur-containing groups 失效
    由含硫基取代的抗高血压5-氨基-4-羟基戊酰基衍生物

    公开(公告)号：US4889869A

    公开(公告)日：1989-12-26

    申请号：US341239

    申请日：1989-04-19

    申请人： Peter Buhlmayer ,  James L. Stanton ,  Walter Fuhrer ,  Richard Goschke ,  Vittorio Rasetti ,  Heinrich Rueger

    发明人： Peter Buhlmayer ,  James L. Stanton ,  Walter Fuhrer ,  Richard Goschke ,  Vittorio Rasetti ,  Heinrich Rueger

    IPC分类号： C07D233/54 ,  C07D233/64 ,  C07D233/84 ,  C07D401/12 ,  C07D417/12

    CPC分类号： C07D233/64 ,  C07D233/84 ,  C07D401/12 ,  C07D417/12 ,  Y10S530/86

    摘要： Compounds of the formula ##STR1## in which R.sub.1 represents acyl substituted by a thio, sulphinyl or sulphonyl group, A represents an optionally N-alkylated .alpha.-amino acid residue that is bonded N-terminally to R.sub.1 and C-terminally to the group --NR.sub.2 --, R.sub.2 represents hydrogen or lower alkyl, R.sub.3 represents hydrogen, lower alkyl, optionally etherified or esterified hydroxy-lower alkyl, cycloalkyl, cycloalkyl-lower alkyl, bicycloalkyl-lower alkyl, tricycloalkyl-lower alkyl, aryl or aryl-lower alkyl, R.sub.4 represents hydroxy or etherified or esterified hydroxy, R.sub.5 represents lower alkyl, optionally etherified or esterified hydroxy-lower alkyl, cycloalkyl, cycloalkyl-lower alkyl, bicycloalkyl, bicycloalkyl-lower alkyl, tricycloalkyl, tricycloalkyl-lower alkyl, aryl, aryl-lower alkyl, optionally substituted carbamoyl, optionally substituted amino, optionally substituted hydroxy, optionally substituted mercapto, sulyhinyl or sulphonyl, and R.sub.6 represents substituted amino, and salts of such compounds having salt-forming groups, inhibit the blood pressure-increasing action of the enzyme renin and can be used as anti-hypertensives.

    摘要翻译： 式（I）的化合物，其中R 1表示被硫代，亚磺酰基或磺酰基取代的酰基，A表示任选N-烷基化的α-氨基酸残基，其N-末端与R1和C-末端键合 基团-NR 2 - ，R 2表示氢或低级烷基，R 3表示氢，低级烷基，任选醚化或酯化的羟基 - 低级烷基，环烷基，环烷基 - 低级烷基，双环烷基 - 低级烷基，三环烷基 - 低级烷基，芳基或芳基 - 低级烷基，R4代表羟基或醚化或酯化的羟基，R5代表低级烷基，任选醚化或酯化羟基 - 低级烷基，环烷基，环烷基 - 低级烷基，双环烷基，双环烷基 - 低级烷基，三环烷基，三环烷基 - 低级烷基，芳基，芳基 - 低级烷基，任选取代的氨基甲酰基，任选取代的氨基，任选取代的羟基，任选取代的巯基，磺酰基或磺酰基，R 6代表取代的氨基， 具有盐形成基团，抑制了肾素素的增压作用，可用作抗高血压药。

    Substituted tetrapeptides
    9.
    发明授权
    Substituted tetrapeptides 失效
    取代四肽

    公开(公告)号：US4595677A

    公开(公告)日：1986-06-17

    申请号：US554735

    申请日：1983-11-23

    申请人： Bernhard Riniker ,  Peter Buhlmayer ,  Walter Fuhrer

    发明人： Bernhard Riniker ,  Peter Buhlmayer ,  Walter Fuhrer

    IPC分类号： A61K38/00 ,  C07K5/02 ,  C07K7/02 ,  C07K7/14 ,  A61K37/02

    CPC分类号： C07K5/0227 ,  C07K7/02 ,  C07K7/14 ,  A61K38/00 ,  Y10S530/86

    摘要： Tetrapeptides of the formula I, ##STR1## in which R.sup.1 represents hydrogen or acyl, R.sup.2 represents alkyl or aralkyl, R.sup.3 represents free or functionally modified hydroxy, R.sup.4 represents free or substituted amino or free or etherified hydroxy, and -Pro-, -Phe- and -His- respectively represent the bivalent radicals of the amino acids proline, phenylalanine and histidine or the (D)-isomers thereof, salts of such compounds having salt-forming groups, and processes for their manufacture.The compounds inhibit the action of the enzyme renin and can be used as antihypertensives and for the treatment of cardiac insufficiency.

    摘要翻译： 式I的四肽，其中R 1表示氢或酰基，R 2表示烷基或芳烷基，R 3表示游离或官能改性的羟基，R 4表示游离或取代的氨基或游离的或醚化的羟基，和-Pro- ，-Phe-和-His-分别表示氨基酸脯氨酸，苯丙氨酸和组氨酸或其（D）异构体的二价基团，这些具有成盐基团的化合物的盐及其制备方法。 该化合物抑制酶肾素的作用，可用作抗高血压药物和治疗心功能不全。

    Benzazepinone derivatives
    10.
    发明授权
    Benzazepinone derivatives 失效

    公开(公告)号：US5610153A

    公开(公告)日：1997-03-11

    申请号：US454106

    申请日：1994-07-12

    申请人： Peter Buhlmayer ,  Pascal Furet

    发明人： Peter Buhlmayer ,  Pascal Furet

    IPC分类号： A61K31/55 ,  A61K31/554 ,  A61P9/00 ,  A61P13/02 ,  A61P15/00 ,  A61P25/00 ,  A61P25/08 ,  A61P25/28 ,  A61P43/00 ,  C07D267/14 ,  C07D281/10 ,  C07D513/04

    CPC分类号： C07D267/14 ,  C07D281/10

    摘要： The invention relates to substituted 3-amino-1-arylalkyl-benzazepin-2-ones of the general formula ##STR1## wherein Ar is aryl;X is --O-- or --S(O).sub.n -- and n is 0, 1 or 2;X.sub.1 is C.sub.1 -C.sub.2 alkylene or a direct bond;R.sub.1 is hydrogen, lower alkyl, aryl-lower alkyl or acyl;R.sub.2 is lower alkyl, hydroxy-lower alkyl, lower alkoxy-lower alkyl, aryl-lower alkoxy-lower alkyl, aryl-lower alkyl or C.sub.3 -C.sub.7 cycloalkyl-lower alkyl;R.sub.3 is carboxy; lower alkoxycarbonyl; lower alkoxy-lower alkoxycarbonyl; aryl-lower alkoxycarbonyl; aryloxycarbonyl; carbamoyl; carbamoyl that (i) is monosubstituted by hydroxy, lower alkanesulfonyl, halo-lower alkanesulfonyl or by arylsulfonyl, (ii) is monosubstituted or disubstituted, the substituents being independent of one another, by lower alkyl, lower alkenyl, lower alkynyl or by phenyl-lower alkyl or (iii) is disubstituted by lower alkylene or by lower alkylene-Z.sub.1 -lower alkylene, Z.sub.1 being O, S or NH; 5-tetrazolyl; PO.sub.2 H.sub.2 ; PO.sub.3 H.sub.2 or SO.sub.3 H.sub.2 ; the ring A and aromatic radicals are, independently of one another, unsubstituted or mono- or poly-substituted by substituents selected from the group consisting of: lower alkyl, aryl-lower alkyl, lower alkoxy-lower alkyl, lower alkoxy, lower alkoxy-lower alkoxy, aryl-lower alkoxy, C.sub.3 -C.sub.7 cycloalkyl, C.sub.3 -C.sub.7 cycloalkyl-lower alkyl, nitro, halogen, trifluoromethyl, amino and amino that is monosubstituted or disubstituted, the substituents being independent of one another, by lower alkyl, aryl-lower alkyl or by aryl, or disubstituted by lower alkylene or by lower alkyleneoxy-lower alkylene;or a salt thereof; to processes for the preparation thereof; and to the use thereof as well as to pharmaceutical compositions that comprise compounds of formula (I) or pharmaceutically acceptable salts thereof.